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Assay Detail

CHEMBL5385387

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of PKD1 (unknown origin) assessed as inhibition constant
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Polycystin-1 (CHEMBL5772)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design.
Crawford JJ, Feng J, Brightbill HD, Johnson AR, Wright M, Kolesnikov A, Lee W, Castanedo GM, Do S, Blaquiere N, Staben ST, Chiang PC, Fan PW, Baumgardner M, Wong S, Godemann R, Grabbe A, Wiegel C, Sujatha-Bhaskar S, Hymowitz SG, Liau N, Hsu PL, McEwan PA, Ismaili MHA, Landry ML.
Bioorg Med Chem Lett (2023) 89 : 129277 -129277
PubMed 37105490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.14 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5405484 1 7.19
CHEMBL4211840 1 7.18
CHEMBL4209095 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5405484 Ki = 64.0 nM 7.19
CHEMBL4211840 Ki = 66.0 nM 7.18
CHEMBL4209095 Ki = 89.0 nM 7.05